2763365-40-6
2763365-40-6 structure
- Name: BPR1R024 mesylate
- Chemical Name: BPR1R024 mesylate
- CAS Number: 2763365-40-6
- Molecular Formula: C25H25F3N6O5S
- Molecular Weight: 578.56
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK c-Fms
- Create Date: 2022-11-26 12:07:07
- Modify Date: 2023-01-16 00:04:11
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BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor.BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology[1].
| Name | BPR1R024 mesylate |
|---|
| Description | BPR1R024 mesylate is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor.BPR1R024 mesylate is the equivalent of BPR1R024 (HY-132935). BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology[1]. |
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| Related Catalog | |
| Target |
IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB)[1]. |
| In Vitro | BPR1R024 (compound 12) has potent CSF1R inhibition activity with an IC50 value of 0.53 nM[1]. BPR1R024 exhibits weake AURA and AURB inhibitory activity in enzyme activity assay with IC50 values of ＞10 μM and 1.40 μM, respeactively[1]. BPR1R024 (0-500 nM) significantly suppressed the CSF1R signal in a dose-dependent manner[1]. BPR1R024 (10 nM, 100 nM) inhibits CSF1/CSF1R signaling-mediated TNF-α production[1]. BPR1R024 (0-10 μM) specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth[1]. Western Blot Analysis[1] Cell Line: RAW264.7 and THP-1 cells Concentration: 0-500 nM Incubation Time: 16 h Result: Significantly suppressed the CSF1R signal in a dose-dependent manner, at concentrations of approximately 50-75 and 1-10 nM in RAW264.7 and THP-1 cells, respectively. |
| In Vivo | BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model[1]. Animal Model: Rats[1] Dosage: 5, 20, 25 mg/kg Administration: IV, PO Result: Exhibited high systemic drug exposure with the dose-normalized area under curve (DNAUC) values of 3635 ng/mL*h by the IV route and 362 ng/mL*h by the PO route and the modification increased oral bioavailability (F=35%). Animal Model: C57BL/6 mice (six-week-old, male)[1] Dosage: 100 mg/kg Administration: Oral, twice a day Result: Delayed the MC38 murine colon tumor growth and reversed the immunosuppressive tumor microenvironment with the increased M1/M2 ratio. |
| Molecular Formula | C25H25F3N6O5S |
|---|---|
| Molecular Weight | 578.56 |